Altiratinib | DCC-2701 | MET/TIE2/VEGFR2/FLT3/Trk Inhibitor

Altiratinib {[allProObj[0].p_purity_real_show]}

货号：A206114 同义名： DCC-2701

Altiratinib是一种 c-MET/TIE-2/VEGFR 抑制剂，能够有效减少体内肿瘤负担，并与 HGF 拮抗剂相比，阻断 c-MET pTyr(1349) 介导的信号传导、细胞生长和迁移。

Altiratinib 化学结构
CAS号：1345847-93-9

Altiratinib 3D分子结构
CAS号：1345847-93-9

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FLT3 亚型比较

VEGFR 亚型比较

产品名称	FLT3 ↓ ↑	其他靶点	纯度
R406	✔	Syk	98%
Go6976	✔		99%+
Quizartinib	+++ FLT3 (ITD), IC50: 1.1 nM FLT3 (WT), IC50: 4.2 nM		98%
Gilteritinib	++++ FLT3, IC50: 0.29 nM		99%+
Amuvatinib	+ FLT3 (D835Y), IC50: 81 nM		99%+
Pacritinib	++ FLT3, IC50: 22 nM FLT3 (D835Y), IC50: 6 nM		97%
Dovitinib	++++ FLT3, IC50: 1 nM	c-Kit	99%+
Denfivontinib	++++ FLT3, IC50: 0.4 nM FLT3 (D835Y), IC50: 0.4 nM	RET	99%+
TAK-659 HCl	++ FLT3, IC50: 4.6 nM	Syk	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	97%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ VEGFR2, IC50: 25 nM Flk1, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	c-Kit,FGFR,PDGFR	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms/CSF1R	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	c-Kit,BTK	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM	+ hVEGFR3, IC50: 420 nM		99%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Apatinib mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Altiratinib 生物活性

描述

Altiratinib is a c-MET/TIE-2/VEGFR inhibitor which effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro.

Altiratinib 细胞实验

Cell Line Ba/F3 TPM3-NTRK1G667S Ba/F3 TPM3-NTRK1G667C Ba/F3 TPM3-NTRK1F589L Ba/F3 TPM3-NTRK1V573M Ba/F3 ETV6-NTRK3G623R Ba/F3 ETV6-NTRK3 Ba/F3 TPM3-NTRK1 GSC6-27, GSC7-2, GSC11, GSC17, GSC231, GSC295, GSC20, GSC300, GSC28, GSC272, GSC8-11, GSC262, GSC23, GSC280 Ba/F3 cells Mouse melanocytes (Mel-Ab) Normal human epidermal melanocytes (NHM) GIC lines (G88 and G528) mouse melanocytes (Mel-Ab) normal human melanocytes (NHM) B16F10 mouse melanoma cells	Concentration	Treated Time	Description	References
Ba/F3 TPM3-NTRK1G667S	93.5 nM	72 h	Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1G667S mutant cells, results show IC50 of 93.5 nM	Commun Biol. 2020 Dec 16;3(1):776.
Ba/F3 TPM3-NTRK1G667C	1.8 nM	72 h	Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1G667C mutant cells, results show IC50 of 1.8 nM	Commun Biol. 2020 Dec 16;3(1):776.
Ba/F3 TPM3-NTRK1F589L	18.3 nM	72 h	Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1F589L mutant cells, results show IC50 of 18.3 nM	Commun Biol. 2020 Dec 16;3(1):776.
Ba/F3 TPM3-NTRK1V573M	2.8 nM	72 h	Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1V573M mutant cells, results show IC50 of 2.8 nM	Commun Biol. 2020 Dec 16;3(1):776.
Ba/F3 ETV6-NTRK3G623R	240 nM	72 h	Evaluate the inhibitory effect of Altiratinib on ETV6-NTRK3G623R mutant cells, results show partial sensitivity with IC50 of 240 nM	Commun Biol. 2020 Dec 16;3(1):776.
Ba/F3 ETV6-NTRK3	7.3 nM	72 h	Evaluate the inhibitory effect of Altiratinib on ETV6-NTRK3 fusion-driven cells, results show IC50 of 7.3 nM	Commun Biol. 2020 Dec 16;3(1):776.
Ba/F3 TPM3-NTRK1	11.3 nM	72 h	Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1 fusion-driven cells, results show IC50 of 11.3 nM	Commun Biol. 2020 Dec 16;3(1):776.
GSC6-27, GSC7-2, GSC11, GSC17, GSC231, GSC295, GSC20, GSC300, GSC28, GSC272, GSC8-11, GSC262, GSC23, GSC280	0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 5 μM	72 h	Determination of cell viability and IC50	Neuro Oncol. 2016 Sep;18(9):1230-41.
Ba/F3 cells	100 nM	72 h	Screening for drugs that inhibit MET D1228A/Y secondary mutations, found that Altiratinib and other four type II MET-TKIs showed growth inhibition below 50%	J Hematol Oncol. 2022 Jun 11;15(1):79.
Mouse melanocytes (Mel-Ab)	0.01–1 µM	72 h	To evaluate the effect of Altiratinib on melanogenesis. Results showed that Altiratinib inhibited FSK-stimulated nuclear localization of CRTC3 by increasing its phosphorylation, thereby reducing melanogenesis.	Theranostics. 2021 Oct 17;11(20):9918-9936.
Normal human epidermal melanocytes (NHM)	0.01–1 µM	72 h	To evaluate the effect of Altiratinib on melanogenesis. Results showed that Altiratinib dose-dependently suppressed FSK-stimulated CREB transcriptional activity and reduced melanin content without affecting cell viability.	Theranostics. 2021 Oct 17;11(20):9918-9936.
GIC lines (G88 and G528)	0–2.5 μM	72 h	To evaluate the effects of altiratinib and abemaciclib alone and in combination on GIC cell viability, showing significant synergy in combination therapy.	Cancer Res. 2018 Aug 1;78(15):4360-4369.
mouse melanocytes (Mel-Ab)	1 µM	72 h	Evaluate effects on tyrosinase activity	Clin Transl Med. 2024 Mar;14(3):e1625.
normal human melanocytes (NHM)	10 µM	72 h	Evaluate cytotoxicity and melanogenesis inhibition	Clin Transl Med. 2024 Mar;14(3):e1625.
B16F10 mouse melanoma cells	1 µM	72 h	Evaluate inhibitory effects on CRTC3 activity and melanogenesis	Clin Transl Med. 2024 Mar;14(3):e1625.

Cell Line

Concentration

Treated Time

Description

References

Ba/F3 TPM3-NTRK1G667S

93.5 nM

72 h

Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1G667S mutant cells, results show IC50 of 93.5 nM

Commun Biol. 2020 Dec 16;3(1):776.

Ba/F3 TPM3-NTRK1G667C

1.8 nM

72 h

Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1G667C mutant cells, results show IC50 of 1.8 nM

Commun Biol. 2020 Dec 16;3(1):776.

Ba/F3 TPM3-NTRK1F589L

18.3 nM

72 h

Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1F589L mutant cells, results show IC50 of 18.3 nM

Commun Biol. 2020 Dec 16;3(1):776.

Ba/F3 TPM3-NTRK1V573M

2.8 nM

72 h

Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1V573M mutant cells, results show IC50 of 2.8 nM

Commun Biol. 2020 Dec 16;3(1):776.

Ba/F3 ETV6-NTRK3G623R

240 nM

72 h

Evaluate the inhibitory effect of Altiratinib on ETV6-NTRK3G623R mutant cells, results show partial sensitivity with IC50 of 240 nM

Commun Biol. 2020 Dec 16;3(1):776.

Ba/F3 ETV6-NTRK3

7.3 nM

72 h

Evaluate the inhibitory effect of Altiratinib on ETV6-NTRK3 fusion-driven cells, results show IC50 of 7.3 nM

Commun Biol. 2020 Dec 16;3(1):776.

Ba/F3 TPM3-NTRK1

11.3 nM

72 h

Evaluate the inhibitory effect of Altiratinib on TPM3-NTRK1 fusion-driven cells, results show IC50 of 11.3 nM

Commun Biol. 2020 Dec 16;3(1):776.

GSC6-27, GSC7-2, GSC11, GSC17, GSC231, GSC295, GSC20, GSC300, GSC28, GSC272, GSC8-11, GSC262, GSC23, GSC280

0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 5 μM

72 h

Determination of cell viability and IC50

Neuro Oncol. 2016 Sep;18(9):1230-41.

Ba/F3 cells

100 nM

72 h

Screening for drugs that inhibit MET D1228A/Y secondary mutations, found that Altiratinib and other four type II MET-TKIs showed growth inhibition below 50%

J Hematol Oncol. 2022 Jun 11;15(1):79.

Mouse melanocytes (Mel-Ab)

0.01–1 µM

72 h

To evaluate the effect of Altiratinib on melanogenesis. Results showed that Altiratinib inhibited FSK-stimulated nuclear localization of CRTC3 by increasing its phosphorylation, thereby reducing melanogenesis.

Theranostics. 2021 Oct 17;11(20):9918-9936.

Normal human epidermal melanocytes (NHM)

0.01–1 µM

72 h

To evaluate the effect of Altiratinib on melanogenesis. Results showed that Altiratinib dose-dependently suppressed FSK-stimulated CREB transcriptional activity and reduced melanin content without affecting cell viability.

Theranostics. 2021 Oct 17;11(20):9918-9936.

GIC lines (G88 and G528)

0–2.5 μM

72 h

To evaluate the effects of altiratinib and abemaciclib alone and in combination on GIC cell viability, showing significant synergy in combination therapy.

Cancer Res. 2018 Aug 1;78(15):4360-4369.

mouse melanocytes (Mel-Ab)

1 µM

72 h

Evaluate effects on tyrosinase activity

Clin Transl Med. 2024 Mar;14(3):e1625.

normal human melanocytes (NHM)

10 µM

72 h

Evaluate cytotoxicity and melanogenesis inhibition

Clin Transl Med. 2024 Mar;14(3):e1625.

B16F10 mouse melanoma cells

1 µM

72 h

Evaluate inhibitory effects on CRTC3 activity and melanogenesis

Clin Transl Med. 2024 Mar;14(3):e1625.

Altiratinib 动物实验

Species Mouse Nude mice BALB/c SCID NCr mice KRT14-SCF transgenic mice	Animal Model NIH3T3 ETV6-NTRK3 xenograft model GSC11 and GSC17 xenograft mouse models Orthotopic GBM xenograft model Skin hyperpigmentation model	Administration	Dosage	Frequency	Description	References
Mouse	NIH3T3 ETV6-NTRK3 xenograft model	Oral	15 mg/kg	Once daily, continuous treatment	Evaluate the inhibitory effect of Altiratinib on ETV6-NTRK3 fusion-driven tumors, results show significant tumor growth inhibition	Commun Biol. 2020 Dec 16;3(1):776.
Nude mice	GSC11 and GSC17 xenograft mouse models	Oral gavage	10 mg/kg	Twice daily, continuous treatment	Evaluate the effects of Altiratinib alone or in combination with bevacizumab on tumor growth, invasiveness, angiogenesis, and TIE2-expressing monocyte infiltration	Neuro Oncol. 2016 Sep;18(9):1230-41.
BALB/c SCID NCr mice	Orthotopic GBM xenograft model	Oral gavage	40 mg/kg; 60 mg/kg	Continuous treatment: abemaciclib 6 days/week, altiratinib daily; Alternating treatment: each drug alternating 3 days on and 3 days off	To evaluate the efficacy of altiratinib and abemaciclib alone and in combination in an orthotopic GBM xenograft model, showing that the combined treatment significantly prolonged median and overall survival.	Cancer Res. 2018 Aug 1;78(15):4360-4369.
KRT14-SCF transgenic mice	Skin hyperpigmentation model	Topical application	10 µM	Not specified	Evaluate inhibition of epidermal melanin and tyrosinase protein levels	Clin Transl Med. 2024 Mar;14(3):e1625.

Species

Mouse Nude mice BALB/c SCID NCr mice KRT14-SCF transgenic mice

Animal Model

NIH3T3 ETV6-NTRK3 xenograft model GSC11 and GSC17 xenograft mouse models Orthotopic GBM xenograft model Skin hyperpigmentation model

Administration

Dosage

Frequency

Description

References

Mouse

NIH3T3 ETV6-NTRK3 xenograft model

Oral

15 mg/kg

Once daily, continuous treatment

Evaluate the inhibitory effect of Altiratinib on ETV6-NTRK3 fusion-driven tumors, results show significant tumor growth inhibition

Commun Biol. 2020 Dec 16;3(1):776.

Nude mice

GSC11 and GSC17 xenograft mouse models

Oral gavage

10 mg/kg

Twice daily, continuous treatment

Evaluate the effects of Altiratinib alone or in combination with bevacizumab on tumor growth, invasiveness, angiogenesis, and TIE2-expressing monocyte infiltration

Neuro Oncol. 2016 Sep;18(9):1230-41.

BALB/c SCID NCr mice

Orthotopic GBM xenograft model

Oral gavage

40 mg/kg; 60 mg/kg

Continuous treatment: abemaciclib 6 days/week, altiratinib daily; Alternating treatment: each drug alternating 3 days on and 3 days off

To evaluate the efficacy of altiratinib and abemaciclib alone and in combination in an orthotopic GBM xenograft model, showing that the combined treatment significantly prolonged median and overall survival.

Cancer Res. 2018 Aug 1;78(15):4360-4369.

KRT14-SCF transgenic mice

Skin hyperpigmentation model

Topical application

10 µM

Not specified

Evaluate inhibition of epidermal melanin and tyrosinase protein levels

Clin Transl Med. 2024 Mar;14(3):e1625.

Altiratinib 参考文献

Altiratinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.80mL

1.96mL

0.98mL

19.59mL

3.92mL

1.96mL

Altiratinib 技术信息

CAS号	1345847-93-9
分子式	C₂₆H₂₁F₃N₄O₄
分子量	510.46
SMILES Code	O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC(F)=C(OC4=CC(NC(C5CC5)=O)=NC=C4)C=C3F
MDL No.	MFCD28900672

别名	DCC-2701
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 25 mg/mL(48.97 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

Altiratinib {[allProObj[0].p_purity_real_show]}

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全球学术期刊中引用的产品

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Altiratinib 动物实验

Altiratinib 参考文献

Altiratinib 实验方案

Altiratinib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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