2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. Calderasib

Calderasib (MK-1084) is a selective KRAS G12C inhibitor. Calderasib exhibits anticancer activity and can be used either alone or in combination with Pembrolizumab (HY-P9902) for cancer research.

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Calderasib

Calderasib 화학구조

CAS No. : 2641216-67-1

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
500 μg 해외재고보유
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg   견적 받기  
200 mg   견적 받기  

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Calderasib Related Antibodies

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  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Calderasib (MK-1084) is a selective KRAS G12C inhibitor. Calderasib exhibits anticancer activity and can be used either alone or in combination with Pembrolizumab (HY-P9902) for cancer research[1].

In Vitro

Calderasib (MK-1084) (0.01-10 μM, 2 h) inhibits the SOS-catalyzed nucleotide exchange with IC50 of 1.2 nM, inhibits the phosphorylation of ERK1/2 in cell H358 with IC50 of 9 nM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Calderasib Related Antibodies
In Vivo

Calderasib (MK-1084) (10-30 mg/kg, po for 14 days) exhibits antitumor efficacy in mouse MiaPaCa-2 xenograft models[2].
Calderasib (MK-1084) exhibits a good pharmacokinetic characteristics with a plasma clearance of 22 mL/min/kg, a mean residence time MRT of 1.1 h and an oral bioavailability of 61%[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse MiaPaCa-2 xenograft models[2]
Dosage: 10-30 mg/kg
Administration: po for 14 days
Result: Inhibited tumor growth.
Clinical Trial
분자량

637.08

화학식

C32H31ClF2N6O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=C2C(OCCOC3=CC=NC(C(C)C)=C3N4C5=NC2=C(Cl)C=C5C(N6[C@@H](C)CN(C(C=C)=O)[C@H](C)C6)=NC4=O)=C(F)C=C1
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

용액&용해도
In Vitro: 

DMSO : 100 mg/mL (156.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5697 mL 7.8483 mL 15.6966 mL
5 mM 0.3139 mL 1.5697 mL 3.1393 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
순도&문서
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5697 mL 7.8483 mL 15.6966 mL 39.2415 mL
5 mM 0.3139 mL 1.5697 mL 3.1393 mL 7.8483 mL
10 mM 0.1570 mL 0.7848 mL 1.5697 mL 3.9242 mL
15 mM 0.1046 mL 0.5232 mL 1.0464 mL 2.6161 mL
20 mM 0.0785 mL 0.3924 mL 0.7848 mL 1.9621 mL
25 mM 0.0628 mL 0.3139 mL 0.6279 mL 1.5697 mL
30 mM 0.0523 mL 0.2616 mL 0.5232 mL 1.3081 mL
40 mM 0.0392 mL 0.1962 mL 0.3924 mL 0.9810 mL
50 mM 0.0314 mL 0.1570 mL 0.3139 mL 0.7848 mL
60 mM 0.0262 mL 0.1308 mL 0.2616 mL 0.6540 mL
80 mM 0.0196 mL 0.0981 mL 0.1962 mL 0.4905 mL
100 mM 0.0157 mL 0.0785 mL 0.1570 mL 0.3924 mL
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Calderasib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Calderasib2641216-67-1MK-1084MK1084MK 1084Rasorally activeselectiveMiaPaCa-2H358Inhibitorinhibitorinhibit

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상품명:
Calderasib
Cat. No.:
HY-162431
수량:
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